Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB

Publication date: Available online 22 October 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Yolanda Pérez-Pertejo, José M. Escudero-Martínez, Rosa M. Reguera, Rafael Balaña-Fouce, Pablo A. García, Pablo G. Jambrina, Arturo San Feliciano, María-Ángeles CastroAbstractLeishmania is the aethiological agent responsible for the visceral leishmaniasis, a serious parasite-borne disease widely spread all over the World. The emergence of resistant strains makes classical treatments less effective; therefore, new and better drugs are necessary. Naphthoquinones are interesting compounds for which many pharmacological properties have been described, including leishmanicidal activity. This work shows the antileishmanial effect of two series of terpenyl-1,4-naphthoquinones (NQ) and 1,4-anthraquinones (AQ) obtained from natural terpenoids, such as myrcene and myrceocommunic acid. They were evaluated both in vitro and ex vivo against the transgenic iRFP-Leishmania infantum strain and also tested on liver HepG2 cells to determine their selectivity indexes. The results indicated that NQ derivatives showed better antileishmanial activity than AQ analogues, and among them, compounds with a diacetylated hydroquinone moiety provided better results than their corresponding quinones. Regarding the terpenic precursor, compounds obtained from the monoterpenoid myrcene displayed good antiparasitic efficiency and low cytotoxicity for mammalian cells, where...
Source: International Journal for Parasitology: Drugs and Drug Resistance - Category: Parasitology Source Type: research